[Federal Register Volume 80, Number 162 (Friday, August 21, 2015)]
[Notices]
[Pages 50858-50859]
From the Federal Register Online via the Government Publishing Office [www.gpo.gov]
[FR Doc No: 2015-20694]


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DEPARTMENT OF HEALTH AND HUMAN SERVICES

National Institutes of Health


Government-Owned Inventions; Availability for Licensing

AGENCY: National Institutes of Health, HHS.

ACTION: Notice.

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SUMMARY: The inventions listed below are owned by an agency of the U.S. 
Government and are available for licensing in the U.S. in accordance 
with 35 U.S.C. 209 and 37 CFR part 404 to achieve expeditious 
commercialization of results of federally-funded research and 
development. Foreign patent applications are filed on selected 
inventions to extend market coverage for companies and may also be 
available for licensing.

FOR FURTHER INFORMATION CONTACT: Licensing information and copies of 
the U.S. patent applications listed below may be obtained by writing to 
the indicated licensing contact at the Office of Technology Transfer, 
National Institutes of Health, 6011 Executive Boulevard, Suite 325, 
Rockville, Maryland 20852-3804; telephone: 301-496-7057; fax: 301-402-
0220. A signed Confidential Disclosure Agreement will be required to 
receive copies of the patent applications.

SUPPLEMENTARY INFORMATION: Technology descriptions follow.

Novel Benztropine Analogs for Treatment of Cocaine Abuse and Other 
Mental Disorders

    Description of Technology: Dopamine is a neurotransmitter that 
exerts important effects on locomotor activity, motivation and reward, 
and cognition. The dopamine transporter (DAT) is expressed on the 
plasma membrane of dopamine synthesizing neurons, and is responsible 
for clearing dopamine released into the extra-cellular space, thereby 
regulating neurotransmission. The dopamine transporter plays a 
significant role in neurotoxicity and human diseases, such as 
Parkinson's disease, drug abuse (especially cocaine addiction), 
Attention Deficit Disorder/Attention Deficit Hyperactivity Disorder 
(ADD/ADHD), and a number of other CNS disorders. Therefore, the 
dopamine transporter is a strong target for research and the discovery 
of potential therapeutics for the treatment of these indications.
    This invention discloses novel benztropine analogs and methods of 
using these analogs for treatment of mental and conduct disorders such 
as cocaine abuse, narcolepsy, ADHD, obesity and nicotine abuse. The 
disclosed analogs are highly selective and potent inhibitors of DAT, 
but without an apparent cocaine-like behavioral profile. In addition to 
their use as a treatment for cocaine abuse, these compounds have also 
shown efficacy in animal models of ADHD and nicotine abuse, and have 
also been shown to reduce food intake in animals. They may also be 
useful medications for other indications where dopamine-related 
behavior is compromised, such as alcohol addiction, tobacco addiction, 
and Parkinson's disease.
    Potential Commercial Applications:
     Drug leads for treatment of cocaine abuse, ADHD, nicotine 
abuse, obesity, and other dopamine-related disorders
     Imaging probes for dopamine transporter binding sites
    Development Stage: Early-stage; In vitro data available
    Inventors: Amy H. Newman, Mu-fa Zou, Jonathan L. Katz (all of NIDA)
    Intellectual Property: HHS Reference No. E-234-2005/1--US Patent 
No. 8,383,817 issued February 26, 2013
    Licensing Contact: Betty B. Tong, Ph.D.; 301-594-6565; 
[email protected]
    Collaborative Research Opportunity: The National Institute on Drug 
Abuse, Medicinal Chemistry and Psychobiology Sections, is seeking 
statements of capability or interest from parties interested in 
collaborative research to further develop, evaluate, or commercialize 
medications to treat cocaine abuse and addiction. For collaboration 
opportunities please contact John D. Hewes, Ph.D. at 
[email protected].

Novel Dopamine Receptor Ligands as Therapeutics for Central Nervous 
System Disorders

    Description of Technology: The dopamine D3 receptor subtype is a 
member of the dopamine D2 subclass of receptors. These receptors have 
been implicated in a number of CNS disorders, including psychostimulant

[[Page 50859]]

abuse, psychosis and Parkinson's disease. Compounds that bind with high 
affinity and selectivity to D3 receptors can not only provide important 
tools with which to study the structure and function of this receptor 
subtype, but may also have therapeutic potential in the treatment of 
numerous psychiatric and neurologic disorders.
    The 4-phenylpiperazine derivatives are an important class of 
dopamine D3 selective ligands. However, due to their highly lipophilic 
nature, these compounds suffer from solubility problems in aqueous 
media and reduced bioavailability. To address this problem, a process 
was designed to introduce functionality into the carbon chain linker of 
these compounds. Compared to currently available dopamine D3 receptor 
ligands, the resulting compounds show improved pharmacological 
properties and D3 selectivities but due to their more hydrophilic 
nature, these derivatives are predicted to have improved water 
solubility and bioavailability.
    Potential Commercial Applications:
     Therapeutics for a variety of psychiatric and neurologic 
disorders
     Research tools to study D3 receptor structure and function
    Competitive Advantages:
     Improved pharmacological properties and selectivity over 
existing dopamine D3 receptor ligands
     Hydrophilic nature likely to lead to improved water 
solubility and bioavailability
    Development Stage: Early-stage; In vitro data available
    Inventors: Amy H. Newman (NIDA), Peter Grundt (NIDA), Jianjing Cao 
(NIDA), Robert Luedtke
    Intellectual Property: HHS Reference No. E-128-2006/0--US Patent 
No. 8,748,608 issued June 10, 2014
    Licensing Contact: Betty B. Tong, Ph.D.; 301-594-6565; 
[email protected]
    Collaborative Research Opportunity: The National Institute on Drug 
Abuse, Medications Discovery Research Branch, is seeking statements of 
capability or interest from parties interested in collaborative 
research to further develop, evaluate, or commercialize 4-
phenylpiperazine derivatives as dopamine D3 selective ligands. For 
collaboration opportunities, please contact Vio Conley, M.S. at 240-
276-5531 or [email protected].

Genome Wide DNase I Hypersensitive Sites Detection in Formalin-Fixed 
Paraffin-Embedded Single Cells

    Description of Technology: A method of detecting DNase I 
hypersensitive sites ((DHS) in a single cell or very small number of 
cells, including cells recovered from formalin-fixed paraffin-embedded 
(FFPE) tissue slides of patient samples. DHS has revealed a large 
number of potential regulatory elements for transcriptional regulation 
in various cell types. The application of DNase-Seq techniques to 
patient samples can elucidate pathophysiological mechanisms of gene 
function in a variety of diseases as well as provide potentially 
important diagnostic and prognostic information. Unfortunately, the 
current DNase-Seq techniques require large number of cells and are 
applicable only to larger biopsies and surgical specimens. This 
technique, called Pico-Seq, allows detection when only very small 
population of cells are available, such as rare primary tumor cells and 
circulating-tumor-cells, isolated by a variety of methods. Pico-Seq 
uses conditions capable of restoring the DNase I sensitivity, similar 
to native/fresh cells, in tissue/cells from slides processed by 
extremely harsh conditions, such as in FFPE tissues.
    Potential Commercial Applications:
     Diagnostic and prognostic kits
     Research kits
    Competitive Advantages:
     Applicable to very small number of cells down to a single 
cell.
     Capable of using cells isolated by any of the available 
methods, including flow cytometry, biopsies, laser capture 
microdissection, and even cells recovered from formalin-fixed paraffin-
embedded tissue slides of patient samples.
    Development Stage: Early-stage; In vitro data available
    Inventors: Keji Zhao and Tang Qingsong (NHLBI)
    Intellectual Property: HHS Reference No. E-254-2014/0--US 
Provisional Application No. 62/118,574 filed February 20, 2015
    Licensing Contact: Cristina Thalhammer-Reyero, Ph.D., M.B.A.; 301-
435-4507; [email protected]

    Dated: August 18, 2015.
Richard U. Rodriguez,
Acting Director, Office of Technology Transfer, National Institutes of 
Health.
[FR Doc. 2015-20694 Filed 8-20-15; 8:45 am]
 BILLING CODE 4140-01-P